Preparation method of linezolid intermediate
A linezolid and body technology, which is applied in the field of preparation of linezolid intermediates, can solve the problems of high equipment requirements, cumbersome process, low yield and the like, and achieves easy industrial production, high reaction total yield and simple process. Effect
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Embodiment 1
[0039] Example 1 (S)-2-((3-(3-fluoro-4-morpholinylphenyl)-2-oxo-5-oxazoline)methyl)isoindole-1,3-dione Preparation of (I-1)
[0040]
[0041] Anhydrous lithium bromide (0.9g) and (S)-2-(oxirane-2-methylene)isoindole-1,3-dione (3.66g) were dissolved in N,N-dimethyl 3-Fluoro-4-morpholine phenyl isocyanate in DMF (4.0 g, 20 mL) was added to methyl formamide (DMF) (30 mL), and reacted at 60° C. for 4 h. 60 mL of water was added to the reaction liquid, filtered, the filter cake was washed with cold petroleum ether (10 mL×2), and dried to obtain 6.90 g of white solid, yield 90.11%.
[0042] ESI-MS (m / z): 426 (M+H), 448 (M+Na);
[0043] 1 HNMR (400MHz, CDCl 3 )δ: 3.04(m, 4H), 3.84(m, 4H), 3.95(m, 2H), 4.08(m, 2H), 4.95(m, 1H), 6.90(t, 1H), 7.1(m, 1H ), 7.37 (dd, 1H), 7.75 (m, 2H), 7.87 (m, 2H).
Embodiment 2
[0044] Example 2 (S)-2-((3-(3-fluoro-4-morpholinylphenyl)-2-oxo-5-oxazoline)methyl)isoindole-1,3-dione preparation of
[0045] Anhydrous lithium bromide (0.9 g) and (S)-2-(oxirane-2-methylene)isoindole-1,3-dione (3.66 g) were dissolved in DMF (30 mL), respectively, A solution of 3-fluoro-4-morpholine phenylisocyanate in DMF (4.0 g, 20 mL) was added and reacted at 100° C. for 4 h. 60 mL of water was added to the reaction solution, filtered, the filter cake was washed with cold petroleum ether (10 mL×2), and dried to obtain 7.10 g of white solid, yield 92.72%.
[0046] ESI-MS (m / z): 426 (M+H), 448 (M+Na);
[0047] 1 HNMR (400MHz, CDCl 3 )δ: 3.04(m, 4H), 3.84(m, 4H), 3.95(m, 2H), 4.08(m, 2H), 4.95(m, 1H), 6.90(t, 1H), 7.1(m, 1H ), 7.37 (dd, 1H), 7.75 (m, 2H), 7.87 (m, 2H).
Embodiment 3
[0048] Example 3 (S)-2-((3-(3-fluoro-4-morpholinylphenyl)-2-oxo-5-oxazoline)methyl)isoindole-1,3-dione preparation of
[0049] Anhydrous lithium bromide (0.9 g) and (S)-2-(oxirane-2-methylene)isoindole-1,3-dione (3.66 g) were dissolved in DMF (30 mL), respectively, A solution of 3-fluoro-4-morpholine phenylisocyanate in DMF (4.0 g, 20 mL) was added and reacted at 115° C. for 4 h. 60 mL of water was added to the reaction liquid, filtered, the filter cake was washed with cold petroleum ether (10 mL×2), and dried to obtain 7.29 g of white solid, yield 95.16%.
[0050] ESI-MS (m / z): 426 (M+H), 448 (M+Na);
[0051] 1 HNMR (400MHz, CDCl 3)δ: 3.04(m, 4H), 3.84(m, 4H), 3.95(m, 2H), 4.08(m, 2H), 4.95(m, 1H), 6.90(t, 1H), 7.1(m, 1H ), 7.37 (dd, 1H), 7.75 (m, 2H), 7.87 (m, 2H).
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